Konorev Pharm Lect Drug Targets

Question 1

what do protein kinases do?

Answer 1

phosphorylate proteins

Question 2

What 2 things are present at a MAJORITY of signal pathways?

Answer 2

Protein kinases and transcription factors

Question 3

what are transcription factors?

Answer 3

proteins that bind to specific DNA sequences and control the transcription of genetic information from DNA to RNA

Question 4

where does a transcription factor bind?

Answer 4

to an enhancer or promoter of DNA adjacent to coding sequence of regulated gene

Question 5

what is the name of the specific DNA sequence that the transcription factor binds to?

Answer 5

response element

Question 6

T/F when a trimeric G-protein is activated the affinity of its Alpha subunit for GTP is decreased?

Answer 6

F

Question 7

what is the other name for a GPCR?

Answer 7

7 transmembrane or 7 pass domain

Question 8

what family of G proteins activate all isoforms of AC and Scr tyrosine kinase?

Answer 8

Gs

Question 9

what G protein family activates phospholipase CB(beta)?

Answer 9

Gq

Question 10

what family of GPCR inhibitis AC 13, 5, 6 but activates tyrosine kinase Src?

Answer 10

Gi

Question 11

What type of molecules do transcription factors interact with to fulfill their main function?

Answer 11

DNA

Question 12

Diacylglycerol is lipophilic intermediate that activates…?

Answer 12

Protein Kinase C

Question 13

which endogenous ligand activates receptor tyrosine kinase?

Answer 13

insulin

Question 14

SH2 domain of RTK binds to?

Answer 14

phosphorylated tyrosines

Question 15

SH3 domain binds to?

Answer 15

the proline-rich sequences

Question 16

which proteins contain a variety of protein-binding domains that link protein partners together and facilitate the creation of larger signaling complexes?

Answer 16

adaptor proteins

Question 17

what kinds of ligands are lipophilic, examples?

Answer 17

steroid hormones, thyroid hormones, Vit A, Vit C, and lipid mediates, free fatty acids and their products

Question 18

permeability to what ion is increased as a result of activation of a nicotinic receptor?

Answer 18

mostly Na+

Question 19

GABA is an inhibitory neurotransmitter as binding of GABA to its cognate receptor ion channel will cause

Answer 19

influx of Cl-

Question 20

voltage gated channels are activated by what?

Answer 20

depolarization of the membrane

Question 21

what composes fast Na+ channels? where are these present?

Answer 21

alpha and beta subunit, all excitable tissue

Question 22

what are some examples of drugs that inhibit voltage-gated Na+ channels?

Answer 22

local anesthetics (lidocaine), antiarrhythmic drugs (quinidine), drugs used to tx epilepsy (phenytoine)

Question 23

A 55yo man with CAD is tx with an antihyperlipidemic drug. Drugs A and B have the same mechanism of lowering the blood lipid levels. Drug A in a dose of 1mg produces the same magnitude of lipid lowering as 20mg of Drug B. what does this suggest?

Answer 23

drug B is more potent

Question 24

A physician considersd two medications Drug A and B to tx her pt. Drug A is a partial agonist

Answer 24

finish this later